Bioorganic & Medicinal Chemistry Letters 2006-05-01

Substituted coumarins as potent 5-lipoxygenase inhibitors.

Erich L Grimm, Christine Brideau, Nathalie Chauret, Chi-Chung Chan, Daniel Delorme, Yves Ducharme, Diane Ethier, Jean-Pierre Falgueyret, Richard W Friesen, Jocelyne Guay, Pierre Hamel, Denis Riendeau, Chantal Soucy-Breau, Philip Tagari, Yves Girard

Index: Bioorg. Med. Chem. Lett. 16(9) , 2528-31, (2006)

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Abstract

Leukotriene biosynthesis inhibitors have potential as therapeutic agents for asthma and inflammatory diseases. A novel series of substituted coumarin derivatives has been synthesized and the structure-activity relationship was evaluated with respect to their ability to inhibit the formation of leukotrienes via the human 5-lipoxygenase enzyme.